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PE20091008A1 - HETEROCYCLIC DERIVATIVES AS MODULATORS OF PHOSPHOINOSITIDE 3-KINASE - Google Patents

HETEROCYCLIC DERIVATIVES AS MODULATORS OF PHOSPHOINOSITIDE 3-KINASE

Info

Publication number
PE20091008A1
PE20091008A1 PE2008001296A PE2008001296A PE20091008A1 PE 20091008 A1 PE20091008 A1 PE 20091008A1 PE 2008001296 A PE2008001296 A PE 2008001296A PE 2008001296 A PE2008001296 A PE 2008001296A PE 20091008 A1 PE20091008 A1 PE 20091008A1
Authority
PE
Peru
Prior art keywords
alkyl
phosphoinositide
modulators
kinase
benzothiazol
Prior art date
Application number
PE2008001296A
Other languages
Spanish (es)
Inventor
Shon Booker
Amico Derin C D
Angelo Noel D
Tae-Seong Kim
Longbin Liu
Kristin Meagher
Mark H Norman
Kathleen Panter
Lorie Schenkel
Adrian L Smith
Nuria A Tamayo
Douglas A Whittington
Ning Xi
Kevin Yang
Original Assignee
Amgen Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of PE20091008A1 publication Critical patent/PE20091008A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

REFERIDA A UN COMPUESTO HETEROCICLICO DE FORMULA (I), DONDE A1 ES CR3 O N; A2 ES CR4 O N; A3 ES CR5 O N; A4 ES CR6 O N; X ES OXIGENO O S; R1 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R2 ES ALQUILO C1-C6-R7a, ALQUENILO C2-C6-R7a, ALQUINILO C2-C6-R7a, ENTRE OTROS; R3, R4, R5 Y R6 SON H, HALO, ALQUILO C1-C8, ENTRE OTROS; R7a ES H, ALQUILO C1-C8, ALQUENILO C2-C8, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(6-(2-(3-(3-PIRIDINIL)PROPOXI)-4-PIRIMIDINIL)-1,3-BENZOTIAZOL-2-IL)ACETAMIDA, N-(6-(2-(3-MORFOLINO)PROPOXI)-4-PIRIMIDINIL)-1,3-BENZOTIAZOL-2-IL)ACETAMIDA, N-(6-(2-(3-PIRIDINIL)ETOXI)-4-PIRIMIDINIL)-1,3-BENZOTIAZOL-2-IL)ACETAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE LA ACTIVIDAD DE LA FOSFOINOSITIDA 3-CINASA (PI3K) Y SON UTILES EN EL TRATAMIENTO DE CARCINOMAS, LEUCEMIAS, GLIOBLASTOMAS, CANCER, ENTRE OTRASREFERRED TO A HETEROCYCLIC COMPOUND OF FORMULA (I), WHERE A1 IS CR3 O N; A2 IS CR4 O N; A3 IS CR5 O N; A4 IS CR6 O N; X IS OXYGEN OR S; R1 IS H, C1-C6 ALKYL, C2-C6 ALKENYL, C2-C6 ALKYL, AMONG OTHERS; R2 IS C1-C6-R7a ALKYL, C2-C6-R7a ALKYL, C2-C6-R7a ALKYL, AMONG OTHERS; R3, R4, R5 AND R6 ARE H, HALO, C1-C8 ALKYL, AMONG OTHERS; R7a IS H, C1-C8 ALKYL, C2-C8 ALKYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE: N- (6- (2- (3- (3-PYRIDINYL) PROPOXY) -4-PYRIMIDINYL) -1,3-BENZOTHIAZOL-2-IL) ACETAMIDE, N- (6- (2- (3 -MORPHOLINO) PROPOXY) -4-PYRIMIDINYL) -1,3-BENZOTHIAZOL-2-IL) ACETAMIDE, N- (6- (2- (3-PYRIDINYL) ETOXY) -4-PYRIMIDINYL) -1,3-BENZOTHIAZOL- 2-IL) ACETAMIDE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE MODULATORS OF THE ACTIVITY OF PHOSPHOINOSITIDE 3-KINASE (PI3K) AND ARE USEFUL IN THE TREATMENT OF CARCINOMAS, LEUKEMIA, GLIOBLASTOMAS, CANCER, AMONG OTHERS

PE2008001296A 2007-08-02 2008-08-01 HETEROCYCLIC DERIVATIVES AS MODULATORS OF PHOSPHOINOSITIDE 3-KINASE PE20091008A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US96326307P 2007-08-02 2007-08-02

Publications (1)

Publication Number Publication Date
PE20091008A1 true PE20091008A1 (en) 2009-08-10

Family

ID=39811462

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001296A PE20091008A1 (en) 2007-08-02 2008-08-01 HETEROCYCLIC DERIVATIVES AS MODULATORS OF PHOSPHOINOSITIDE 3-KINASE

Country Status (11)

Country Link
US (1) US7928140B2 (en)
EP (1) EP2183232B1 (en)
JP (1) JP5561702B2 (en)
AR (1) AR068051A1 (en)
AU (1) AU2008282728B2 (en)
CA (1) CA2694136C (en)
CL (1) CL2008002294A1 (en)
ES (1) ES2401557T3 (en)
PE (1) PE20091008A1 (en)
TW (1) TW200911798A (en)
WO (1) WO2009017822A2 (en)

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EP2183232A2 (en) 2010-05-12
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